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Product Infomation
Product NamePNU-200577
CAS No.

207679-81-0

Molecular Weight

341.49

Formula

C₂₂H₃₁NO₂

SMILES

OC1=C(C=C(CO)C=C1)[C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C

Stock statusGet quote



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Product description

Description

Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively[1]. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053)[2][3]. Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats[4].


IC50 & Target

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Kb: 0.84 nM (mAChR)[1].


In Vitro

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In vitro, Desfesoterodine preventes carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner[1].
In radioligand binding studies carries out in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors, Desfesoterodine is not selective for any muscarinic receptor subtype[1].




Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month







Peferences:

[1]. Nilvebrant L, Gillberg PG, Sparf B. Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol. 1997 Oct;81(4):169-72.

[2]. Fullhase, Claudius; Soler, Roberto; Gratzke, Christian et al. Spinal effects of the fesoterodine metabolite 5-hydroxymethyl tolterodine and/or doxazosin in rats with or without partial urethral obstruction. Journal of Urology (New York, NY, United States) (2010), 184(2), 783-789.

[3]. B Malhotra, et al. The Design and Development of Fesoterodine as a Prodrug of 5-hydroxymethyl Tolterodine (5-HMT), the Active Metabolite of Tolterodine. Curr Med Chem. 2009;16(33):4481-9.

[4]. Naoki Aizawa, et al. Selective Inhibitory Effect of Imidafenacin and 5-hydroxymethyl Tolterodine on Capsaicin Sensitive C Fibers of the Primary Bladder Mechanosensitive Afferent Nerves in the Rat. J Urol. 2015 Apr;193(4):1423-32.